Activity-Based Imaging Probes of the Proteasome

Kimberly Cornish Carmony, Kyung Bo Kim

Research output: Contribution to journalArticlepeer-review

16 Scopus citations


Over the years, the proteasome has been extensively investigated due to its crucial roles in many important signaling pathways and its implications in diseases. Two proteasome inhibitors-bortezomib and carfilzomib-have received FDA approval for the treatment of multiple myeloma, thereby validating the proteasome as a chemotherapeutic target. As a result, further research efforts have been focused on dissecting the complex biology of the proteasome to gain the insight required for developing next-generation proteasome inhibitors. It is clear that chemical probes have made significant contributions to these efforts, mostly by functioning as inhibitors that selectively block the catalytic activity of proteasomes. Analogues of these inhibitors are now providing additional tools for visualization of catalytically active proteasome subunits, several of which allow real-time monitoring of proteasome activity in living cells as well as in in vivo settings. These imaging probes will provide powerful tools for assessing the efficacy of proteasome inhibitors in clinical settings. In this review, we will focus on the recent efforts towards developing imaging probes of proteasomes, including the latest developments in immunoproteasome-selective imaging probes.

Original languageEnglish
Pages (from-to)91-101
Number of pages11
JournalCell Biochemistry and Biophysics
Issue number1
StatePublished - Sep 2013

Bibliographical note

Funding Information:
Acknowledgments We gratefully acknowledge the National Institutes of Health for their financial support (R01 CA128903).


  • Activity-based inhibitors
  • Immunoproteasome
  • Proteasome
  • Subunit-selective imaging probe

ASJC Scopus subject areas

  • Biophysics
  • Biochemistry
  • Cell Biology


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